Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6- tetrahydropyridines as 5-HT2C agonists
A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor studied to determine whether either series showed noteworthy agonist activity. Structure-activity relationships were developed from the performed receptor binding assays and functional studies, and the results of the analysis are presented herein.
Conway, Richard J.,Valant, Celine,Christopoulos, Arthur,Robertson, Alan D.,Capuano, Ben,Crosby, Ian T.
supporting information; experimental part
p. 2560 - 2564
(2012/05/05)
4-ARYLMORPHOLIN-3-ONE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE THEREOF
The invention relates to compounds corresponding to formula (I): in which: Ar represents a mono- or disubstituted phenyl; R1 represents an unsubstituted or substituted phenyl; R2 represents: a pyridyl; an unsubstituted or substituted phenyl; a benzyl that is unsubstituted or substituted on the phenyl; R2 may moreover represent: a heterocyclic radical; R3 represents various values. The invention also comprises methods for the compounds preparation, formulations comprising them and therapeutic applications thereof.
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Page/Page column 29
(2008/06/13)
Modulators of dopamine neurotransmission
A 3-substituted 4-(phenyl-N-alkyl)-piperazine compound of the following formula: wherein R1 is selected from the group consisting of OSO2CF3, OSO2CH3, SO2R3, COCF3, CO
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Page/Page column 13
(2008/06/13)
Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; Preparation process and therapeutic application.
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Page/Page column 10
(2008/06/13)
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